Antimalarials. 10. Synthesis of 4-substituted primaquine analogs as candidate antimalarials

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Abstract
Primaquine (I) is extensively used in combination with other drugs in the radical cure of relapsing malaria and for prophylaxis or interruption of transmission. This, coupled with activity data reported for 4-methylprimaquine (II) led to the synthesis of a series of 14 4-substituted analogs of I. Side-chain analogs (3) of II were prepared. Compounds were tested for suppressive antimalarial activity against Plasmodium berghei in the Rane mouse screen and for radical curative activity against P. cynomolgi in the rhesus monkey. Of the 17 compounds prepared, 4 exhibited activity in at least 1 test system.